The novel anticonvulsant SE 204269 binds to a stereospecific site in the mouse brain

被引：9

作者：

Herdon, H ^{[1
]}

Jerman, J ^{[1
]}

Stean, T ^{[1
]}

Chan, W ^{[1
]}

Middlemiss, D ^{[1
]}

Upton, N ^{[1
]}

机构：

[1] SMITHKLINE BEECHAM PHARMACEUT,DEPT MED CHEM,HARLOW CM19 5AW,ESSEX,ENGLAND

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1996年 / 314卷 / 03期

关键词：

anticonvulsant; brain binding site; SB; 204269;

D O I：

10.1016/S0014-2999(96)00737-6

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The novel compound SB 204269 (trans-(+)-6-acetyl-4S-(4-fluorobenzoylamino)-3,4-dihydro-2,2-dimethyl-2H-benzo[b]pyran-3R-ol, hemihydrate) shows potent anticonvulsant activity in the mouse maximal electroshock seizure threshold test. The binding of [H-3]SB 204269 to mouse forebrain membranes is saturable (B-max 217 fmol/mg protein, K-d 32 nM) and stereospecific. The excellent anticonvulsant profile of SE 204269, combined with the identification of a unique central binding site for the compound, suggest that it has potential clinical utility as a novel treatment for epilepsy.

引用

页码：R7 / R8

页数：2

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